About: Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties

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About: Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties Goto Sponge Distinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://dx.doi.org/10.1016/j.bmcl.2011.08.042
Description	Cholinesterase inhibitors are, so far, the only successful strategy for the symptomatic treatment of Alzheimer's disease. Tacrine (THA) is a potent acetylcholinesterase inhibitor that was used in the treatment of Alzheimer's disease for a long time. However, the clinical use of THA was hampered by its low therapeutic index, short half-life and liver toxicity. 7-methoxytacrine (7-MEOTA) is equally pharmacological active compound with lower toxicity compared to THA. In this paper, the synthesis, biological activity and molecular modelling of elimination by-product isolated during synthesis of 7-MEOTA based bis-alkylene linked compound is described. Cholinesterase inhibitors are, so far, the only successful strategy for the symptomatic treatment of Alzheimer's disease. Tacrine (THA) is a potent acetylcholinesterase inhibitor that was used in the treatment of Alzheimer's disease for a long time. However, the clinical use of THA was hampered by its low therapeutic index, short half-life and liver toxicity. 7-methoxytacrine (7-MEOTA) is equally pharmacological active compound with lower toxicity compared to THA. In this paper, the synthesis, biological activity and molecular modelling of elimination by-product isolated during synthesis of 7-MEOTA based bis-alkylene linked compound is described. (en)
Title	Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties (en)
skos:prefLabel	Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties (en)
skos:notation	RIV/60162694:G44__/11:00002428!RIV13-GA0-G44_____
http://linked.open...avai/riv/aktivita	P S Z
http://linked.open...avai/riv/aktivity	P(GAP303/11/1907), S, Z(MSM0021620849)
http://linked.open...iv/cisloPeriodika	21
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Kuča, Kamil Musílek, Kamil Píša, Libor
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ministerstvo obrany / Univerzita obrany - Fakulta vojenského zdravotnictví Hradec Králové
http://linked.open...dnocenehoVysledku	233871
http://linked.open...ai/riv/idVysledku	RIV/60162694:G44__/11:00002428
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	inhibition selectivity; molecular modelling; butyrylcholinesterase; Alzheimer disease; acetylcholinesterase; 7-methoxytacrine (en)
http://linked.open.../riv/klicoveSlovo	7-methoxytacrine inhibition selectivity Alzheimer disease acetylcholinesterase butyrylcholinesterase molecular modelling
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[06A420AD599A]
http://linked.open...i/riv/nazevZdroje	Bioorganic & Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	3 (xsd:int)
http://linked.open...cetTvurcuVysledku	11 (xsd:int)
http://linked.open...vavai/riv/projekt	Novel inhibitors of acetylcholinesterase derived from 7-MEOTA - potential Alzheimer´s disease drugs
http://linked.open...UplatneniVysledku	2011
http://linked.open...v/svazekPeriodika	21
http://linked.open...iv/tvurceVysledku	Fišar, Zdeněk Hroudová, Jana Jung, Young-Sik Kuča, Kamil Musílek, Kamil Zemek, Filip Korábečný, Jan Opletalová, Veronika Holas, Ondřej Horová, Anna Nepovimova, Eugenie
http://linked.open...ain/vavai/riv/wos	000296025900071
http://linked.open...n/vavai/riv/zamer	Neuropsychiatrické aspekty neurodegenerativních onemocnění
issn	0960-894X
number of pages	4 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.bmcl.2011.08.042
http://localhost/t...ganizacniJednotka	G44

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